ChEMBL ligand: CHEMBL75169
A1 receptor/Adenosine receptor A1 in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] There should be some charts here, you may need to enable JavaScript!
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274] A2A receptor/Adenosine receptor A2a in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] There should be some charts here, you may need to enable JavaScript!
A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] There should be some charts here, you may need to enable JavaScript!
ABCB1/ATP-dependent translocase ABCB1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] There should be some charts here, you may need to enable JavaScript!
ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
A1 receptor/Adenosine receptor A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Binding affinity at Adenosine A1 receptor in rat brain membranes by [3H]PIA displacement.	B	4.56	pKi	27600	nM	Ki	J Med Chem (1996) 39: 2293-2301 [PMID:8691424]
ChEMBL	Displacement of specific [3H]PIA binding from adenosine A1 receptor in rat brain membranes.	B	4.56	pKi	27600	nM	Ki	J Med Chem (1996) 39: 781-788 [PMID:8576921]
GtoPdb	-	-	4.6	pKi	-	-	-	J Med Chem (1996) 39: 2293-301 [PMID:8691424]
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb	-	-	4.3	pKi	-	-	-	J Med Chem (1996) 39: 2293-301 [PMID:8691424]
A2A receptor/Adenosine receptor A2a in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Affinity at Adenosine A2A receptor in rat striatal membranes by [3H]- CGS 21680 displacement.	B	4.33	pKi	46700	nM	Ki	J Med Chem (1996) 39: 781-788 [PMID:8576921]
A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Binding affinity against human adenosine A3 receptor in HEK293 cells using [125I]AB-MECA 21680 radioligand.	B	5.58	pKi	2650	nM	Ki	J Med Chem (1996) 39: 2293-2301 [PMID:8691424]
ChEMBL	Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells	B	5.58	pKi	2650	nM	Ki	J Med Chem (1996) 39: 781-788 [PMID:8576921]
ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	B	4.57	pIC50	27100	nM	IC50	Eur J Med Chem (2013) 67: 115-126 [PMID:23851114]
ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay	B	5.22	pIC50	5980	nM	IC50	Eur J Med Chem (2013) 67: 115-126 [PMID:23851114]
ChEMBL	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry	B	5.23	pIC50	5940	nM	IC50	Eur J Med Chem (2013) 67: 115-126 [PMID:23851114]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]